title: In vitro sortase A inhibitory and antimicrobial activity of flavonoids isolated from the roots of Sophora flavescens.
abstract: A series of flavonoids (1-14) was isolated from the roots of Sophora flavescens. We evaluated their ability to inhibit both microbial growth and sortase A, an enzyme that plays a key role in cell wall protein anchoring and virulence in Staphylococcus aureus. Most prenylated flavonoids (7-13) displayed potent inhibitory activity against gram-positive and gram-negative bacteria except E. coli, with minimum inhibitory concentrations values ranging from 4.40 to 27.7 μM, and weak or no activity against fungal strains tested. Kurarinol (6) was a potent inhibitor of sortase A, with an IC(50) value of 107.7 ± 6.6 μM. A preliminary structure-activity relationship, including essential structural requirements, is described.
authors.affiliation: College of Pharmacy, Seoul National University, Seoul, Korea.
authors.forename: Ikhoon
authors.initials: I
authors.lastname: Oh
authors.forename: Woo-Young
authors.initials: WY
authors.lastname: Yang
authors.forename: Soon-Chun
authors.initials: SC
authors.lastname: Chung
authors.forename: Tae-Yoon
authors.initials: TY
authors.lastname: Kim
authors.forename: Ki-Bong
authors.initials: KB
authors.lastname: Oh
authors.forename: Jongheon
authors.initials: J
authors.lastname: Shin
mesh_terms: D019881:Aminoacyltransferases / Q000037:antagonists & inhibitors*; D000890:Anti-Infective Agents / Q000032:analysis / Q000302:isolation & purification / Q000494:pharmacology*; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors*; D003546:Cysteine Endopeptidases; D004353:Drug Evaluation, Preclinical; D004926:Escherichia coli / Q000187:drug effects; D005419:Flavonoids / Q000032:analysis / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D018517:Plant Roots; D054876:Prenylation; D029909:Sophora / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000890:Anti-Infective Agents; D001426:Bacterial Proteins; D005419:Flavonoids; C526229:kurarinol; D019881:Aminoacyltransferases; C120542:sortase A; D003546:Cysteine Endopeptidases